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filingDate 2013-02-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2014-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber SG-11201403216U-A
titleOfInvention Methods and compounds useful in the synthesis of orexin-2 receptor antagonists
abstract (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 22 August 2013 (22.08.2013) WIPOIPCT (10) International Publication Number WO 2013/123240 A1 (51) International Patent Classification: C07C 29/147 ( 2006.01) C07C 303/28 (2006.01) C07D 239/28 (2006.01) C12P 41/00 (2006.01) C07C 33/50 (2006.01) C07C 309/70 (2006.01) C07D 239/34 (2006.01) C07D 401/12 (2006.01) (21) International Application Number: PCT/US2013/026204 (22) International Filing Date: (25) Filing Language: (26) Publication Language: 14 February 2013 (14.02.2013) English English (30) Priority Data: 61/600,109 17 February 2012 (17.02.2012) US (71) Applicant: EISAI R&D MANAGEMENT CO., LTD [JP/JP]; 6-10 Koishikawa, 4-Chome Bunkyo-ku, Tokyo, 112-8088 (JP). (72) Inventors; and (71) Applicants (for US only): MONIZ, George, Anthony [US/US]; 700 Huron Avenue, Apt. 18K, Cambridge, MA 02138 (US). WILCOXEN, Annie, Zhu [US/US]; 18 Peter Road, North Reading, MA 01864 (US). BENAYOUD, Farid [US/US]; 805 Forest Streeet, North Andover, MA 01845 (US). LEE, Jaemoon [KR/US]; 57 Argilla Road, Andover, MA 01810 (US). ZHANG, Huiming [CN/US]; 2 Dorset Circle, Andover, MA 01810 (US). TERAUCHI, Taro [JP/JP]; c/o Eisai Co., Ltd. Tsukuba Research, Labor­ atories 1-3 Tokodai 5-chome, Tsukuba-shi, lbaraki (JP). TAKEMURA, Ayumi [JP/JP]; c/o Eisai Co., Ltd. Tsukuba Research, Laboratories 1-3 Tokodai 5-chome, Tsukuba-shi, lbaraki (JP). YOSHIDA, Yu [JP/JP]; c/o Eisai Co., Ltd. Tsukuba Research, Laboratories 1-3 Tokodai 5-chome, Tsukuba-shi, lbaraki (JP). TANAKA, Toshiaki [JP/JP]; c/o Eisai Co., Ltd. Tsukuba Research, Laboratories 1-3 Tokodai 5-chome, Tsukuba-shi, lbaraki (JP). SORIMACHI, Keiichi [JP/JP]; c/o Eisai Co., Ltd. Tsukuba Research, Laboratories 1-3 Tokodai 5-chome, Tsukuba-shi, lbara (JP). NAOE, Yoshimitsu [JP/JP]; c/o Eisai Co., Ltd. Tsukuba Research, Laboratories 1-3 Tokodai 5-chome, Tsukuba-shi, lbaraki (JP). KAZUTA, Yuji [JP/JP]; c/o Eisai Co., Ltd. Tsukuba Research, Labor­ atories 1-3 Tokodai 5-chome, Tsukuba-shi, lbaraki (JP). (74) Agent: MYERS BIGEL SIBLEY & SAJOVEC, P.A.; P.O. Box 37428, Raleigh, NC 27627 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) © •t CJ m CJ i-H o CJ (54) Title: METHODS AND COMPOUNDS USEFUL IN THE SYNTHESIS OF OREXIN-2 RECEPTOR ANTAGONISTS 5 (57) Abstract: The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.
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